Peet N P, Baugh L E, Sunder S, Lewis J E
J Med Chem. 1985 Mar;28(3):298-302. doi: 10.1021/jm00381a007.
A group of 1,4-dihydro-4-oxoquinoline-2- and -3-carboxylic acid esters with nitrogen functionality at the 8-position was synthesized, and 6-oxo-6H-imidazo[4,5,1-ij]quinoline-4- and -5-carboxylic acid esters were elaborated from these. Several of the compounds displayed activity in the rat passive cutaneous anaphylaxis (PCA) test for antiallergic activity. However, PCA activity in this series was accompanied by rat toxicity, as measured by a decrease in percent of normal weight gain over a 2-week period, following a single oral dose.
合成了一组在8位具有氮官能团的1,4 - 二氢 - 4 - 氧代喹啉 - 2 - 和 - 3 - 羧酸酯，并由此制备了6 - 氧代 - 6H - 咪唑并[4,5,1 - ij]喹啉 - 4 - 和 - 5 - 羧酸酯。其中几种化合物在大鼠被动皮肤过敏反应（PCA）试验中表现出抗过敏活性。然而，该系列化合物的PCA活性伴随着大鼠毒性，通过单次口服给药后2周内正常体重增加百分比的下降来衡量。
